ABSTRACT
OBJECTIVE@#Bergenia ciliata (Haw.) Sternb. is used in the Indian traditional system of medicine to treat various ailments including rheumatism and to heal wounds. The objective of the present study was to perform a preclinical characterization of the B. ciliata-based botanical extract IIIM-160.@*METHODS@#IIIM-160 was chemically standardized and analyzed for heavy metal content, aflatoxins, pesticides and microbial load. The in vitro and in vivo efficacies were determined in suitable models of inflammation, arthritis and nociception. An acute oral toxicity study was performed in Swiss albino mice. A suitable oral formulation was developed and characterized.@*RESULTS@#Bergenin was found to be the major component (9.1% w/w) of IIIM-160. The botanical lead displayed inhibition of lipopolysaccharide-induced production of proinflammatory cytokines in THP-1 cells, with selectivity toward interleukin-6 (IL-6) and had an excellent safety-window. It showed anti-inflammatory, anti-arthritic and antinociceptive activity in animal models and was not toxic at oral doses up to 2 g/kg in Swiss-albino mice. The gastroretentive, sustained-release capsule formulation showed sustained-release of the bergenin over the period of 24 h, resulting in improved plasma-exposure of bergenin in Sprague-Dawley rats.@*CONCLUSION@#The dual-activity of IL-6 inhibition and antinociception marks the suitability of IIIM-160 for treating rheumatoid arthritis. This study will serve as the benchmark for further research on this botanical formulation.
ABSTRACT
Background: COPD is a major cause of health care burden worldwide and leading cause of death that is increasing in prevalence. Methylxanthines are used in the treatment of patients with asthma and COPD. Doxofylline (methylxanthine) shows improved disease control, reduced total daily dose of inhaled b2 agonists and improved patient compliance.Methods: This was a prospective, open labelled, randomized, two-arm, parallel group, controlled, clinical trial. 115 patients were randomized to two groups. Patients in group A received tablet doxofylline 400mg BD whereas patients in group B received tablet doxofylline 800mg SR for 4 weeks. Primary outcome measure of trial was change in FEV1 and secondary outcome measure were change in FVC/FEV1, change in symptoms score, effect on health-related quality of life (HRQOL) and safety of study medication.Results: At 4 week the FEV1increase by 13.028% and 17.647% in group A and B respectively. In group A FEV1/FVC increase by 5.79% and in group B it increases by 9.57% at 4 weeks. The symptom score of cough decrease by 77.35% and 97.43% in group A and group B respectively at 4 weeks. In group A shortness of breath decrease by 77.60% and in group B it decreases by 95.90% at 4 weeks. Tightness in chest decrease by 86.29% and 98.40% in group A and group B respectively at 4 weeks.Conclusions:Doxofylline 800mg sustained release tablet provided significantly greater improvement in FEV1, symptomatic control and health related quality of life compared to doxofylline 400mg.